从Hedyotis diffusa中获得17种具有抗炎作用的未经描述的虹膜衍生物及其结构-活性关系
Ling-Feng Qin1, Huan-Huan Gao1, Xu Zhang1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
来自Hedyotis diffusa的新型虹膜衍生物显示出显著的抗炎作用潜力. 具有长链异质部分的化合物在细胞分析中有效降低了氧化的产量.
科学领域:
- 自然产品化学 自然产品化学
- 药理学 药理学是指药理学的学科.
- 药用化学 医学化学
背景情况:
- 赫迪奥蒂斯 (Hedyotis diffusa Willd.) 是一个散的植物. 是一种传统的药用草本.
- 虹膜衍生物已知具有多种生物活性.
- 了解H. diffusa的化学成分和生物活性至关重要.
研究的目的:
- 从Hedyotis diffusa.中分离和表征新的虹膜衍生物.
- 评估分离化合物的抗炎活性.
- 为了研究色素衍生物的结构-活性关系.
主要方法:
- 使用色谱技术分离化合物.
- 通过综合光谱方法 (UV,IR,HRESIMS,CD,NMR) 阐明结构.
- 在体外抗炎测定使用脂聚糖诱导的RAW 264.7细胞来测量氧化的产量.
主要成果:
- 他们分离了17种新的虹膜衍生物 (1-17) 和4种已知的化合物 (18-21).
- 1-8的化合物具有独特的长链亚利法酸部分,在虹膜类动物中是新鲜的.
- 化合物2,4和6显著抑制了氧化的产生 (IC50值:5.69,6.16,6.84μM).
结论:
- 从Hedyotis diffusa.鉴定出具有独特结构的新型虹膜衍生物.
- 特定的化物衍生物通过抑制氧化的产生,表现出强大的抗炎活性.
- 在C-10处的长链异质部分可能是抗炎作用的关键结构特征,这表明H. diffusa是抗炎剂的来源.
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